| Bioactivity | TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control[1]. |
| Target | Ki: 0.47 nM (DOR), 36.56 nM (MOR) and 5.31 nM (KOR)Kb: 0.21 nM (DOR), 9.43 nM (MOR) and 7.18 nM (KOR) |
| In Vivo | TAN-452 (1, 3, 10 mg/kg for p.o. or 0.3, 1, 3 mg/kg for s.c.) suppresses morphine-induced emesis in ferrets[1]. TAN-452 (30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV) has a T1/2 of 2.1 hours[1]. TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner. Administration of TAN-452 at 30 mg/kg alone does not affect SIT[1]. TAN-452 (10, 30 mg/kg; s.c.) significantly suppresses morphine-induced antinociception 30 min after administration. TAN-452 (po) produces no effect up to 300 mg/kg[1]. Animal Model: |
| Name | TAN-452 |
| CAS | 892039-23-5 |
| Formula | C29H30N2O5 |
| Molar Mass | 486.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Tsutomu Suzuki, et al. Pharmacological profile of TAN-452, a novel peripherally acting opioid receptor antagonist for the treatment of opioid-induced bowel syndromes. Life Sci. 2018 Dec 15;215:246-252. |